Effect of PPlD-1, a Synthetic Antiplatelet Compound, on Rabbit Platelets

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  • Liao Chang-Hui
    Pharmacological Institute, College of Medicine, National Taiwan University
  • Ko Feng-Ning
    Pharmacological Institute, College of Medicine, National Taiwan University
  • Kuo Sheng-Chu
    Graduate Institute of Pharmaceutical Chemistry, China Medical College
  • Teng Che-Ming
    Pharmacological Institute, College of Medicine, National Taiwan University

書誌事項

タイトル別名
  • Effect of PP1D-1, a Synthetic Antiplatelet Compound, on Rabbit Platelets.
  • Effect of PP1D-1 a Synthetic Antiplatel

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抄録

The antiplatelet mechanism of a synthetic compound, 2-chloro-3-methoxycarbonylpropionamido-1, 4-naphthoquinone (PP1D-1), was studied by employing washed rabbit platelets in vitro. PP1D-1 concentration-dependently inhibited thrombin (0.1 U/ml)-, platelet-activating factor (2 ng/ml)-, collagen (10 μg/ml)-, arachidonic acid (100 μM)- and U46619 (1 μM)-induced aggregation and ATP release in washed rabbit platelets. The IC50 values of PP1D-1 for aggregation induced by the above inducers are 17.9±1.7, 9.8±1.1, 3.9±0.4, 1.8±0.3 and 1.7±0.3 μM, respectively. PP1D-1 did not affect platelet thromboxane B2 or prostaglandin D2 formation induced by arachidonic acid, indicating that it did not affect cyclooxygenase and thromboxane synthase activities. PP1D-1 significantly inhibited the formation of inositol 1, 4, 5-trisphosphate caused by these five platelet stimulators. Moreover, PP1D-1 inhibited the increase in intracellular calcium concentration induced by these agents. On the contrary, PP1D-1 did not inhibit thapsigargin-elevated intracellular calcium concentration in indomethacin-pretreated platelets, indicating it did not influence the effect of thapsigargin. According to these data, PP1D-1 exerts antiplatelet effects mainly by inhibiting phosphoinositide turnover.

収録刊行物

  • Jpn.J.Pharmacol.

    Jpn.J.Pharmacol. 76 (2), 141-148, 1998

    公益社団法人 日本薬理学会

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